pH-responsive nanoparticles for endosomal targeting

Abstract

It has been recently demonstrated that Neurokinin 1 receptor (NK1R) endosomal signalling participates in pain transmission and it has therefore been proposed that endosomal NK1R signalling is a potential therapeutic target. This work explores this concept, through the design and characterisation of polymeric nanoparticles that selectively deliver the NK1R antagonist Aprepitant into endosomes without disrupting physiological cell function. This strategy utilises the acidic pH environment of the endosomal network to promote nanoparticle disassembly and endosome-selective cargo release, thereby successfully decreasing NK1R-mediated signalling pathways that are associated with pain transmission.